Tebideutorexant
Based on 1 Customer Validation
Tebideutorexant is an OX1R-selective inhibitor with oral bioavailability and blood-brain barrier permeability, with human OX1R pKi 8.17 and rat OX1R pKi 8.13.Tebideutorexant selectively modulates OX1R, with no significant functional effect on OX2R. Tebideutorexant can be used for the research of panic and anxiety disorders.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.95%
- CAS. Nr.: 1637681-55-0
- Formel: C23H16D2F4N4O2
- Molecular Weight:460.42
-
Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Alle Orexin Receptor (OX Receptor) Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Vero C1008 | IC50 |
>2.0 × 105M
Compound: COVC-2283598831
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
10.6019/CHEMBL4651402 |
Tebideutorexant (0.1-10 mg/kg; p.o.) shows dose- and time-dependent brain OX1R occupancy in rats, with oral bioavailability and brain penetration[1].
Tebideutorexant (10 mg/kg; p.o.) reduces NREM and REM sleep latency without altering total sleep duration in rats[1].
Tebideutorexant (30 mg/kg; p.o.) selectively promotes REM sleep in OX2R KO mice, demonstrating in vivo OX1R target engagement[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (male, 300-400 g)[1]
-
Dosage:3, 10, 30 mg/kg
-
Administration:p.o., single dose
-
Result:Blocked CO₂-induced reduction in social interaction behaviors at 10 and 30 mg/kg; attenuated CO₂-induced bradycardia responses at 8 and 9 minutes post-challenge at 30 mg/kg.
-
Animal Model:Sprague-Dawley (male, 300-400 g)[1]
-
Dosage:0.1, 1, 10 mg/kg
-
Administration:p.o., single dose
-
Result:Produced time- and dose-dependent brain OX1R occupancy; reached 89% maximal occupancy at 15 minutes and remained above 47% for 8 hours at 10 mg/kg; achieved plasma EC50 of 34 ng/mL for 50% occupancy.
-
Animal Model:Sprague-Dawley (male, 350-450 g)[1]
-
Dosage:10 mg/kg
-
Administration:p.o., single dose
-
Result:Did not alter total NREM or REM sleep duration; significantly decreased NREM and REM sleep latency.
-
Animal Model:C57Bl6 OX2R knockout (male, 30-35 g, OX2R KO model)[1]
-
Dosage:30 mg/kg
-
Administration:p.o., single dose
-
Result:Significantly reduced REM sleep latency; prolonged REM sleep duration in the first 2 hours post-treatment; showed no effect on NREM sleep parameters.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
-
CAS. Nr. 1637681-55-0
-
Unlabeled Cas 1628320-31-9
-
Appearance Solid
-
Molecular Weight 460.42
-
Formel C23H16D2F4N4O2
-
Color White to off-white
-
SMILES
O=C(C1=C(C2=NC=CC=N2)C(F)=CC=C1)N3[C@@H]4[C@@H](C[C@H](C3([2H])[2H])C4)OC5=CC=C(C=N5)C(F)(F)F
-
Synonyms
JNJ-61393215
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
-
Data Sheet (273 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Tebideutorexant Related Classifications
HY-147403S Related Classifications
Powered by Bioz